A. V. Bogatskii

Character of correlation between the anticonvulsant action of phenazepam and its level in the mouse brain

: The effect of low doses of haloperidol was studied by means of screening and electrophysiological tests. In doses of 0.05--0.15 mg/Kg haloperidol exerts an activating effect which manifests in the elevation of motility, in the potentiation of the convulsant effect of bicuculline, EEG desynchronization and decrement of test response depression in the recovery cycle of the somatosensory primary response. The data obtained suggest that the activating effect of haloperidol is due to the weakening of inhibitory processes in the brain.

Benzo(a)pyrene hydroxylase activity of immunocompetent cells

A study was made of aryl hydrocarbon hydroxylase activity in immunocompetent cells of varying origin and in hepatocytes from CBA mice. The cells from intact animals may be arranged in the following way with regard to the activity of the enzyme: macrophages greater than hepatocytes much greater than thymocytes greater than splenocytes. The immunostimulants (tilorone and its analogs) altered benzo(a)pyrene hydroxylase activity depending on the cell type.

Kinetics of [14C]phenazepam excretion in albino rats after single and repeated injections of the drug

During the 5 days after intraperitoneal injection of [14C] phenazepam into albino rats, both intact animals and animals previously receiving phenazepam injections for 15 days, about 77% of the total radioactivity was excreted with the urine and feces. The excretion processes can be described by a first-order equation. The rate of total excretion of phenazepam was identical after single or repeated injections of the drug. Meanwhile, after a single injection of phenazepam into the animals, it was excreted mainly with the urine, whereas after repeated injections it was excreted mainly with the feces. The process of excretion of phenazepam with the urine after repeated injection is biexponential in character.

Metabolism of nitrazepam in the intestine of albino rats

In the rat intestine nitrazepam is transformed to an amine and acetamide. In the duodenum and small intestine the reduction of nitrazepam and its subsequent acetylation are catalyzed by enzymes in the mucosa. In the cecum and large intestine these processes are due to the action of the microflora and tissue enzymes, and in the rectum to the action of the microflora alone.

The use of dispersion analysis to estimate the anticonvulsant activity of 1,4-benzodiazepines in mice

It has been shown that under the influence of stressors, including nociceptive stimuli, an increase in the concentration of endogenous opioid peptides, especially

Changes in postsynaptic excitation processes in the presence of the Soviet benzodiazepine derivative phenazepam

-endorphin, is observed in the blood of animals (rats [3], rabbits [5]). These substances are known to be capable of inhibiting various autonomic systems of the body, including the cardiovascular and respiratory systems [2]. These facts suggest that endogenous opioid peptides may play an important role in the formation of disturbances of activity of autonomic systems under the influence of shock-producing factors. This is shown by blocking of the development of electronociceptive shock observed in rabbits in the present experiments, and also by results indicating an improvement in the state of rats during hypovolemic and endotoxic shock, and in dogs with hypovolemic shock after administration of antagonists of endogenous opioid peptides [i, 4]. Injection of naloxone into animals with marked hypotension, due not to the shock-producing factor but to injection of reserpine, was ineffective.

Intrahepatic circulation of14C-phenazepam and its metabolites in albino rats

The new psychotropic drug phenazepam inhibits spike discharges of neurons composing the visceral ganglion of the garden snailHelix aspersa and depresses excitatory postsynaptic potentials arising in response to application of acetylcholine to the membrane of the isolated neuron. The parameters of the electrically excitable membrane remain basically unchanged. It is suggested that one possible mechanism of the manifestation of the pharmacological action of the drug may be depression of postsynaptic excitation of the cholinergic receptor membrane.